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This book is a printed edition of the Special Issue entitled “Anticancer Agents: Design, Synthesis and Evaluation” that was published in Molecules. Two review articles and thirty research papers are included in the Special Issue. Three second-generation androgen receptor antagonists that have been approved by the U.S. FDA for the treatment of prostate cancer have been reviewed. Identification of mimics of protein partners as protein-protein interaction inhibitors via virtual screening has been summarized and discussed. Anticancer agents targeting various protein targets, including IGF-1R, Src, protein kinase, aromatase, HDAC, PARP, Toll-Like receptor, c-Met, PI3Kdelta, topoisomerase II, p53, and indoleamine 2,3-dioxygenase, have been explored. The analogs of three well-known tubulin-interacting natural products, paclitaxel, zampanolide, and colchicine, have been designed, synthesized, and evaluated. Several anticancer agents representing diverse chemical scaffolds were assessed in different kinds of cancer cell models. The capability of some anticancer agents to overcome the resistance to currently available drugs was also studied. In addition to looking into the in vitro ability of the anticancer agents to inhibit cancer cell proliferation, apoptosis, and cell cycle, in vivo antitumor efficacy in animal models and DFT were also investigated in some papers.
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Keywords
- 1,2,3-triazole
- 3,6-dibromocarbazole
- 4-(pyridin-4-yloxy)benzamide
- 5-bromoindole
- 5-fluorouracil
- ABCB1 (P-glycoprotein)
- Actin
- ADME
- allene
- amides/esters
- androgen receptor
- anti-cancer activity
- anti-neuroinflammation
- anti-ovarian cancer
- anti-tumor
- anticancer
- anticancer activity
- anticancer agent
- anticancer agents
- anticancer compounds
- antimitotic agents
- antioxidant activity
- antiproliferative activity
- antiproliferative agent
- antitumor
- antitumor activity
- apalutamide
- Apoptosis
- aromatase
- benzimidazole
- benzofurans
- benzofuran–pyrazole
- beta-lapachone
- bivalency
- Breast cancer
- c-Met
- carbazole
- Cell Cycle
- chemical synthesis
- chemoresistance
- chrysin analogues
- colchiceine
- colchicine amide
- colchicine analogs
- colchicine sulfonamide
- colon cancer
- computational docking
- coumarin
- Crystal structure
- cyanopyridone
- cytotoxic activity
- cytotoxic properties
- Cytotoxicity
- darolutamide
- DFT study
- dihydroartemisinin
- dihydropyranoindole
- docking
- docking studies
- Drug Discovery
- drug resistance
- E-stereoselective
- enzalutamide
- enzyme inhibition
- estrone derivatives
- flavonoid
- Flavonoids
- gemcitabine
- HDAC inhibitors
- HeLa
- HepG2
- hydrates
- hydrazine
- IGF-1R
- IL-12
- immune modulation
- indoleamine 2,3-dioxygenase
- Inflammation
- inhibitor
- K562
- kinase inhibitor
- MCF-7
- MDM2-p53 interaction
- medicine
- migration
- mimetics
- molecular simulation
- MOLT-4
- multidrug resistance (MDR) reversal
- N-substituted pyrazoline
- Nanoparticles
- natural product
- Neuroblastoma
- NIH3T3
- o-nitro-benzyl
- organosilicon compounds
- ortho-quinones
- ovarian cancer
- overcoming drug resistance
- P-Glycoprotein
- P-MAPA
- PARP inhibitor
- PARP-1 inhibition
- phenylpyrazolopyrimidine
- photoactivatable protecting groups
- PI3Ks
- PI3Kα inhibitor
- PI3Kδ inhibitors
- polyvalency
- prodrug
- prostate cancer
- PROTACs
- protein degradation
- protein kinase
- protein–protein interactions
- Pyrazole
- pyrazolopyridine
- pyridotriazine
- quinazolin-4(3H)-one
- quinazolin-4(3H)-thione
- regioselective
- salinomycin
- Schiff base
- SILA-409 (Alis-409)
- SILA-421 (Alis-421)
- src
- substituted pyridine
- synergy
- Synthesis
- Talazoparib
- tanshione IIA
- taxoids
- thiazolidinone
- Thienopyrimidine
- thienopyrimidinone
- thiocolchicine
- thiopene
- thioxotriazopyridine
- TLR signaling
- topoisomerase II inhibitor
- triazolothiadiazine
- triple-negative breast cancer
- tryptophan metabolism
- tubulin inhibitors
- tumor specificity
- urea
- virtual screening
- Xanthones
- yeast-based assays
- zampanolide
- βIII-tubulin
Links
DOI: 10.3390/books978-3-0365-0141-3Editions